TABLE 2

EC50 values of methamphetamine and amphetamine for hOCT1 and hOCT2 determined by two-binding site fitting

The EC50 values were obtained by fitting inhibition data in Fig. 1 and Supplemental Fig. 2 using eq. 2 described in Materials and Methods with the fit shown in Supplemental Fig. 3. The last column lists the P values obtained by comparing eqs. 1 and 2 with an extra sum-of-squares F test. Results represent mean ± S.D. of three independent experiments each run in triplicate.

InhibitorTwo-Binding SiteTwo-Binding versus One-Binding Site
TransporterEC50 Value
High AffinityLow Affinity
μMμM
MethamphetaminehOCT15.29 ± 0.66400 ± 229P < 0.0001
hOCT21.21 ± 0.1958.2 ± 23.4P < 0.0001
AmphetaminehOCT1NANAP = 0.55
hOCT20.72 ± 0.29145 ± 104P < 0.0001
  • NA, not applicable.